WO2015157559A3 - 10',11'-modified saxitoxins useful for the treatment of pain - Google Patents

10',11'-modified saxitoxins useful for the treatment of pain Download PDF

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Publication number
WO2015157559A3
WO2015157559A3 PCT/US2015/025182 US2015025182W WO2015157559A3 WO 2015157559 A3 WO2015157559 A3 WO 2015157559A3 US 2015025182 W US2015025182 W US 2015025182W WO 2015157559 A3 WO2015157559 A3 WO 2015157559A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
modified
pain
mammal
saxitoxins
Prior art date
Application number
PCT/US2015/025182
Other languages
French (fr)
Other versions
WO2015157559A2 (en
Inventor
Hassan Pajouhesh
George Miljanich
John Mulcahy
Justin Du Bois
Matthew AXTMAN
James Walker
Jeffrey E. Merit
Original Assignee
Siteone Therapeutics, Inc.
The Board Of Trustees Of The Leland Stanford Junior University
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Siteone Therapeutics, Inc., The Board Of Trustees Of The Leland Stanford Junior University filed Critical Siteone Therapeutics, Inc.
Priority to CA2944549A priority Critical patent/CA2944549A1/en
Priority to US15/302,964 priority patent/US10106549B2/en
Priority to AU2015243437A priority patent/AU2015243437B2/en
Priority to EP15777365.6A priority patent/EP3129381B1/en
Publication of WO2015157559A2 publication Critical patent/WO2015157559A2/en
Publication of WO2015157559A3 publication Critical patent/WO2015157559A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Provided herein are compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function, for example conditions associated with pain. The compounds are 10',11'-modified saxitoxins. The compounds are optionally additionally modified at carbon 13. In certain embodiments, the 10',11'-modified saxitoxins are of Formula I: where R1, R2 and R3 are as described herein. Also provided herein are methods of treating pain in a mammal comprising administering an effective treatment amount of a 10',11' modified saxitoxin or composition to a mammal. In an embodiment, the mammal is a human.
PCT/US2015/025182 2014-04-09 2015-04-09 10',11'-modified saxitoxins for the treatment of pain WO2015157559A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
CA2944549A CA2944549A1 (en) 2014-04-09 2015-04-09 10',11'-modified saxitoxin useful for the treatment of pain
US15/302,964 US10106549B2 (en) 2014-04-09 2015-04-09 10′,11′-modified saxitoxins useful for the treatment of pain
AU2015243437A AU2015243437B2 (en) 2014-04-09 2015-04-09 10',11'-modified saxitoxins useful for the treatment of pain
EP15777365.6A EP3129381B1 (en) 2014-04-09 2015-04-09 10',11'-modified saxitoxins useful for the treatment of pain

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461977494P 2014-04-09 2014-04-09
US61/977,494 2014-04-09

Publications (2)

Publication Number Publication Date
WO2015157559A2 WO2015157559A2 (en) 2015-10-15
WO2015157559A3 true WO2015157559A3 (en) 2016-01-14

Family

ID=54288547

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2015/025182 WO2015157559A2 (en) 2014-04-09 2015-04-09 10',11'-modified saxitoxins for the treatment of pain

Country Status (5)

Country Link
US (1) US10106549B2 (en)
EP (1) EP3129381B1 (en)
AU (1) AU2015243437B2 (en)
CA (1) CA2944549A1 (en)
WO (1) WO2015157559A2 (en)

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JP2018534270A (en) 2015-09-30 2018-11-22 サイトワン セラピューティクス， インコーポレイテッド 11,13-modified saxitoxin for the treatment of pain
GB201602576D0 (en) 2016-02-12 2016-03-30 Bergen Teknologioverforing As Process
US11279706B2 (en) 2017-03-29 2022-03-22 Siteone Therapeutics, Inc. 11,13-modified saxitoxins for the treatment of pain
AU2018243463C1 (en) * 2017-03-29 2022-12-01 Siteone Therapeutics, Inc. 11,13-modified saxitoxins for the treatment of pain
TW202128675A (en) 2019-12-06 2021-08-01 美商維泰克斯製藥公司 Substituted tetrahydrofurans as modulators of sodium channels
AU2022286511A1 (en) 2021-06-04 2023-11-30 Vertex Pharmaceuticals Incorporated Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels
EP4347584A1 (en) 2021-06-04 2024-04-10 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels
CA3221938A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran analogs as modulators of sodium channels
EP4346818A1 (en) 2021-06-04 2024-04-10 Vertex Pharmaceuticals Incorporated Solid dosage forms and dosing regimens comprising (2r,3s,4s,5r)-4-[[3-(3,4-difluoro-2-methoxy-phenyl)-4,5-dimethyl-5-(trifluoromethyl) tetrahydrofuran-2-carbonyl]amino]pyridine-2-carboxamide
CA3221788A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels
US11827627B2 (en) 2021-06-04 2023-11-28 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides as modulators of sodium channels
WO2023205468A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2023205463A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2023205778A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2023205465A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain

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WO2011098539A1 (en) * 2010-02-10 2011-08-18 Phytotox Limited Treatment of loss of sense of touch with saxitoxin derivatives

Also Published As

Publication number Publication date
WO2015157559A2 (en) 2015-10-15
EP3129381B1 (en) 2020-11-04
US10106549B2 (en) 2018-10-23
EP3129381A2 (en) 2017-02-15
US20170029431A1 (en) 2017-02-02
AU2015243437B2 (en) 2019-08-29
AU2015243437A1 (en) 2016-10-20
CA2944549A1 (en) 2015-10-15

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